Results 121 to 130 of about 55,819 (261)

The Isolated Thumb Domain of Acid‐Sensing Ion Channels Forms a Minimal Folding Unit Enabling Ligand Binding Studies

Angewandte Chemie, Volume 138, Issue 19, 4 May 2026.
An independently folded thumb domain from acid‐sensing ion channels (ASICs) preserves ligand‐binding and proton‐sensing properties. NMR‐based interaction and pKa analyses uncover how endogenous and exogenous peptides modulate ASICs, providing a simplified model for rational drug discovery targeting proton‐gated ion channels.
Biswa P. Mishra, Ben Cristofori‐Armstrong, Elena Budusan, Mimi Golder, Neville J. Butcher, Junyu Liu, Theo Crawford, Yanni K.‐Y. Chin, Anneka Pereira Schmidt, Xinying Jia, Taylor B. Smallwood, Richard J. Clark, Jan P. Wurm, Lachlan D. Rash, Mehdi Mobli   +14 more
wiley   +2 more sources

How to Identify a Pharmacophore

Chemistry & Biology, 2008
The inhibition of chitinases by argifin and progressively dissected analogs had been studied by a combination of kinetic and crystallographic methods (Andersen et al., 2008). This work also leads to a general understanding of structure-activity relationships for inhibitors with one distinct pharmacophor.
openaire   +3 more sources

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

British Journal of Pharmacology, EarlyView.
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi, Jamie Cowley, Ashley Pegg, Alison J. Cooper, John Gordon, Catherine A. Brady, Antonio Belli, Sam Butterworth, Rachel Upthegrove, Nick Andrews, Nicholas M. Barnes   +10 more
wiley   +1 more source

In Silico Analysis for Exploring the Potential Inhibitors Against Breast Cancer (MCF7) Using Curcumin Analogue Compounds

Jurnal Kimia Sains dan Aplikasi
Breast cancer is one of the most problematic diseases in the world. Currently, there are no potential vaccines for the treatment of this disease. Therefore, finding effective compounds, such as curcumin analogs, is crucial to inhibit breast cancer. Forty-
Neni Frimayanti, Adel Zamri, Yum Eryanti
doaj   +1 more source

Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways

British Journal of Pharmacology, EarlyView.
Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck, Mario van der Stelt   +1 more
wiley   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Defining AV2‐1 as a novel pharmacological probe to target human and rodent TRPV2

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Transient receptor potential vanilloid 2 (TRPV2) is a non‐selective cation channel implicated in immune cell functions. However, progress in understanding TRPV2 has been limited by a lack of potent and selective pharmacological tools, particularly those targeting the human variant. We aimed to identify and characterise a
Andrea Leipe, Julia A. Rocereta, Ruth A. Pumroy, Andreas Leffler, Michael Schaefer, Vera Moiseenkova‐Bell, Kerstin Hill   +6 more
wiley   +1 more source

A Curcumin‐Derived HSP70 Inhibitor Disrupts Lysosomal Function to Suppress Triple‐Negative Breast Cancer Progression

Cell Proliferation, EarlyView.
Novel curcumin‐derived M4 binds HSP70's ATPase domain, disrupting HSP70‐mediated lysosomes‐autophagy pathway to inhibit TNBC growth and metastasis, and synergizes with paclitaxel for potent combination therapy. ABSTRACT Structural modification of curcumin yielded a novel series of 1,4‐pentadien‐3‐one oxime ether derivatives, among which compound M4 ...
Zijian Li, Wanxia Wang, Yuxin Zhou, Tao Zeng, Jian Liu, Yingjie Qing, Xuan Han   +6 more
wiley   +1 more source

Enzymatic synthesis of bioactive quinolones and (thio)coumarins by fungal type III polyketide synthases

The FEBS Journal, EarlyView.
Quinolones are valuable scaffolds for drug discovery but are rare in nature. Here, we show that two fungal enzymes, AthePKS and FerePKS, can generate 2‐quinolones and two additional heteroaromatic scaffolds. Using AthePKS, we designed an artificial enzymatic cascade towards an antimicrobial quinolone from a simple precursor and implemented it in E ...
Nika Sokolova, Angelina Osipyan, Lili Zhang, Matthew R. Groves, Sandy Schmidt, Kristina Haslinger   +5 more
wiley   +1 more source

Asymmetric Transformations of α,β‐Unsaturated Oxazolidinones Catalyzed by C2‐Symmetric Chiral Iron Triad Complexes

Advanced Synthesis &Catalysis, Volume 368, Issue 9, 5 May 2026.
This review highlights the evolution of highly enantioselective oxazolidinone transformations enabled by C2‐symmetric ligands, with emphasis on chiral iron triad complexes as cost‐effective, environmentally benign alternatives to late‐transition‐metal catalysts.
Arthur David, Thierry Ollevier
wiley   +1 more source